A-966492

Product Name: A-966492
CAS No.: 934162-61-5
Chemical Name: A-966492
Synonyms: CS-903;A-966492;A-966492, >=98%;A-966492 USP/EP/BP;A-966492(A 966492);A966492;A 966492;A-966492;A-966492 PARP inhibitor A966492;2-[2-Fluoro-4-[(2S)-2-pyrrolidinyl]phenyl]-1H-benzimidazole-7-carboxamide;2-[2-fluoro-4-[(2S)-pyrrolidin-2-yl]phenyl]-1H-benzimidazole-4-carboxamide;1H-Benzimidazole-7-carboxamide, 2-[2-fluoro-4-[(2S)-2-pyrrolidinyl]phenyl]-
CBNumber: CB42522977
Molecular Formula: C18H17FN4O
Formula Weight: 324.35
MOL File: 934162-61-5.mol

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A-966492 Property

Boiling point:: 605.5±65.0 °C(Predicted)
Density: 1.335
storage temp.: Store at -20°C
solubility: ≥32.4 mg/mL in DMSO; ≥16.53 mg/mL in H2O with ultrasonic; ≥3.16 mg/mL in EtOH with gentle warming and ultrasonic
form: solid
pka: 9.33±0.30(Predicted)

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Warning

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 26378
Product name: A-966492
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 26378
Product name: A-966492
Packaging: 25mg
Price: $533
Updated: 2024/03/01

Cayman Chemical

Product number: 26378
Product name: A-966492
Packaging: 5mg
Price: $139
Updated: 2024/03/01

Cayman Chemical

Product number: 26378
Product name: A-966492
Packaging: 10mg
Price: $261
Updated: 2024/03/01

ApexBio Technology

Product number: A4160
Product name: A-966492
Packaging: 50mg
Price: $590
Updated: 2021/12/16

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A-966492 Chemical Properties,Usage,Production

Uses

A-966492 effectively inhibits PARP-1 with an EC50 of 1 nM and a Ki value of 1 nM. When it acts on PARP-2, the Ki value is 1.5 nM. It has excellent efficacy on PARP enzyme, especially on C41 cells. A-966492 significantly enhanced the effect of TMZ in a dose-dependent manner.

Biological Activity

a-966492 is an inhibitor of parp-1 with ki value of 1nm [1].parp-1 belongs to the poly(adp-ribose) polymerases (parps) family, it contributes to the resistance happened after cancer therapy. a-966492 is a potent inhibitor of both parp-1 and parp-2 (ki value of 1.5nm) with good potency in c41 whole cells (ec50 value of 1nm). a-966492 shows excellent pharmaceutical properties with oral bioavailabilities of 34-72% and half-lives of 1.7-1.9 h. additionally, a-966492 can crosses the blood-brain barrier. a-966492 is proved potent in a murine b16f10 syngeneic melanoma model and a brca1-deficient mx-1 breast carcinoma model. meanwhile, it can enhance the efficacy of tmz and carboplatin in these models [1].

Synthesis

A-966492 is prepared by reacting 3-Carboxamido-1,2-phenylenediamine with benzoic acid in a solution(methanol:water=1:1) at 50 °C for 2 hours.

References

[1] penning td, zhu gd, gong j, thomas s, gandhi vb, liu x, shi y, klinghofer v, johnson ef, park ch, fry eh, donawho ck, frost dj, buchanan fg, bukofzer gt, rodriguez le, bontcheva-diaz v, bouska jj, osterling dj, olson am, marsh kc, luo y, giranda vl. optimization of phenyl-substituted benzimidazole carboxamide poly(adp-ribose) polymerase inhibitors: identification of (s)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1h-benzimidazole-4-carboxamide (a-966492), a highly potent and efficacious inhibitor. j med chem. 2010 apr 22;53(8):3142-53.

A-966492 Preparation Products And Raw materials

Raw materials

Preparation Products

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A-966492 Suppliers

China 84 United Kingdom 1 United States 16 Global 101

Anqing YanZhi Pharma Discovery Co.,Ltd.

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934162-61-5, A-966492Related Search:

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A966492;A 966492;A-966492

CS-903

A-966492

2-[2-Fluoro-4-[(2S)-2-pyrrolidinyl]phenyl]-1H-benzimidazole-7-carboxamide

A-966492(A 966492)

2-{2-fluoro-4-[(2S)-pyrrolidin-2-yl]phenyl}-1H-1,3-benzodiazole-7-carboxaMide

2-[2-Fluoro-4-[(2S)-2-pyrrolidinyl]phenyl]-1H-benzimidazole-7-carboxamide A-966492

A-966492, >=98%

1H-Benzimidazole-7-carboxamide, 2-[2-fluoro-4-[(2S)-2-pyrrolidinyl]phenyl]-

A-966492 USP/EP/BP

A-966492 PARP inhibitor A966492

2-[2-fluoro-4-[(2S)-pyrrolidin-2-yl]phenyl]-1H-benzimidazole-4-carboxamide

(S)-2-(2-Fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzo[d]imidazole-7-carboxamide

934162-61-5

931462-61-5

Inhibitor

Inhibitors

APIs